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Discovery of a novel alpha-7 nicotinic acetylcholine receptor agonist series and characterization of the potent, selective, and orally efficacious agonist 5-(4-acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H-pyrazol-3-yl] amide (SEN15924, WAY-361789).
Zanaletti R, Bettinetti L, Castaldo C, Cocconcelli G, Comery T, Dunlop J, Gaviraghi G, Ghiron C, Haydar SN, Jow F, Maccari L, Micco I, Nencini A, Scali C, Turlizzi E, Valacchi M. Zanaletti R, et al. Among authors: jow f. J Med Chem. 2012 May 24;55(10):4806-23. doi: 10.1021/jm300247y. Epub 2012 May 3. J Med Chem. 2012. PMID: 22468936
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).
Ghiron C, Haydar SN, Aschmies S, Bothmann H, Castaldo C, Cocconcelli G, Comery TA, Di L, Dunlop J, Lock T, Kramer A, Kowal D, Jow F, Grauer S, Harrison B, La Rosa S, Maccari L, Marquis KL, Micco I, Nencini A, Quinn J, Robichaud AJ, Roncarati R, Scali C, Terstappen GC, Turlizzi E, Valacchi M, Varrone M, Zanaletti R, Zanelli U. Ghiron C, et al. Among authors: jow f. J Med Chem. 2010 Jun 10;53(11):4379-89. doi: 10.1021/jm901692q. J Med Chem. 2010. PMID: 20465311
N-[5-(5-fluoropyridin-3-yl)-1H-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): a medicinal chemistry effort toward an α7 nicotinic acetylcholine receptor agonist preclinical candidate.
Zanaletti R, Bettinetti L, Castaldo C, Ceccarelli I, Cocconcelli G, Comery TA, Dunlop J, Genesio E, Ghiron C, Haydar SN, Jow F, Maccari L, Micco I, Nencini A, Pratelli C, Scali C, Turlizzi E, Valacchi M. Zanaletti R, et al. Among authors: jow f. J Med Chem. 2012 Nov 26;55(22):10277-81. doi: 10.1021/jm3013568. Epub 2012 Nov 2. J Med Chem. 2012. PMID: 23083093
Preclinical assessment of an adjunctive treatment approach for cognitive impairment associated with schizophrenia using the alpha7 nicotinic acetylcholine receptor agonist WYE-103914/SEN34625.
Marquis KL, Comery TA, Jow F, Navarra RL, Grauer SM, Pulicicchio C, Kelley C, Brennan JA, Roncarati R, Scali C, Haydar S, Ghiron C, Terstappen GC, Dunlop J. Marquis KL, et al. Among authors: jow f. Psychopharmacology (Berl). 2011 Dec;218(4):635-47. doi: 10.1007/s00213-011-2357-6. Epub 2011 Jun 4. Psychopharmacology (Berl). 2011. PMID: 21643676
Old and new pharmacology: positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/C) receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']di pyrrole-1(2H)-carboxamide).
Dunlop J, Lock T, Jow B, Sitzia F, Grauer S, Jow F, Kramer A, Bowlby MR, Randall A, Kowal D, Gilbert A, Comery TA, Larocque J, Soloveva V, Brown J, Roncarati R. Dunlop J, et al. Among authors: jow f. J Pharmacol Exp Ther. 2009 Mar;328(3):766-76. doi: 10.1124/jpet.108.146514. Epub 2008 Dec 2. J Pharmacol Exp Ther. 2009. PMID: 19050173
28 results